发现吡唑并嘧啶类化合物是高亲和力烟酸受体GPR109A的第一类变构激动剂。
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
作者信息
Shen Hong C, Taggart Andrew K P, Wilsie Larissa C, Waters M Gerard, Hammond Milton L, Tata James R, Colletti Steven L
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA.
出版信息
Bioorg Med Chem Lett. 2008 Sep 15;18(18):4948-51. doi: 10.1016/j.bmcl.2008.08.039. Epub 2008 Aug 14.
PMID:18752940
Abstract
Pyrazolopyrimidines were discovered as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. In addition to its intrinsic activity, compound 9n significantly enhances nicotinic acid binding to the receptor, thereby potentiating the functional efficacy of nicotinic acid.
摘要
吡唑并嘧啶被发现是高亲和力烟酸受体GPR109A的第一类变构激动剂。除了其内在活性外，化合物9n还能显著增强烟酸与该受体的结合，从而增强烟酸的功能效力。
Zotero 插件